Vicasinabin

Vicasinabin
Identifiers
	IUPAC name (3S)-1-[5-tert-butyl-3-[(1-methyltetrazol-5-yl)methyl]triazolo[4,5-d]pyrimidin-7-yl]pyrrolidin-3-ol;
CAS Number	1433361-02-4;
PubChem CID	86296048;
ChemSpider	115010437;
UNII	QJ8UO6C05M;
KEGG	D12511;
ChEMBL	ChEMBL5314566;
Chemical and physical data
Formula	C15H22N10O
Molar mass	358.410 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)(C)C1=NC2=C(C(=N1)N3CC[C@@H](C3)O)N=NN2CC4=NN=NN4C;
	InChI InChI=1S/C15H22N10O/c1-15(2,3)14-16-12(24-6-5-9(26)7-24)11-13(17-14)25(21-19-11)8-10-18-20-22-23(10)4/h9,26H,5-8H2,1-4H3/t9-/m0/s1; Key:MAYZWDRUFKUGGP-VIFPVBQESA-N;

Vicasinabin (RG7774) is a potent cannabinoid agonist which is highly selective for the CB₂ receptor subtype. It was developed by Roche as a potential agent for the treatment of diabetic retinopathy. It reached Phase II human clinical trials but was discontinued for lack of efficacy, although it continues to be used for scientific research.^[1]^[2]

References

^ Grether U, Foxton RH, Gruener S, Korn C, Kimbara A, Osterwald A, et al. (2024). "RG7774 (Vicasinabin), an orally bioavailable cannabinoid receptor 2 (CB2R) agonist, decreases retinal vascular permeability, leukocyte adhesion, and ocular inflammation in animal models". Frontiers in Pharmacology. 15: 1426446. doi:10.3389/fphar.2024.1426446. PMC 11272598. PMID 39070793.
^ Armendariz BG, Luhman UF, Berger B, Hernandez-Sanchez J, Bogman K, Mitrousis N, et al. (2025). "CANBERRA: A Phase II Randomized Clinical Trial to Test the Therapeutic Potential of Oral Vicasinabin in Diabetic Retinopathy". Ophthalmology Science. 5 (2): 100650. doi:10.1016/j.xops.2024.100650. PMC 11719906. PMID 39802207.

[1] Grether U, Foxton RH, Gruener S, Korn C, Kimbara A, Osterwald A, et al. (2024). "RG7774 (Vicasinabin), an orally bioavailable cannabinoid receptor 2 (CB2R) agonist, decreases retinal vascular permeability, leukocyte adhesion, and ocular inflammation in animal models". Frontiers in Pharmacology. 15: 1426446. doi:10.3389/fphar.2024.1426446. PMC 11272598. PMID 39070793.

[2] Armendariz BG, Luhman UF, Berger B, Hernandez-Sanchez J, Bogman K, Mitrousis N, et al. (2025). "CANBERRA: A Phase II Randomized Clinical Trial to Test the Therapeutic Potential of Oral Vicasinabin in Diabetic Retinopathy". Ophthalmology Science. 5 (2): 100650. doi:10.1016/j.xops.2024.100650. PMC 11719906. PMID 39802207.

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